ArticleExperimental parasitology2011
Quercetin, a fluorescent bioflavanoid, inhibits Trypanosoma brucei hexokinase 1.
Article in Experimental parasitology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 33 citations in OpenAlex.
- In Vitro Study on the Efficacy of Ziziphus vulgaris L. and Camellia sinensis (L.) Kuntze Extracts for Controlling Varroa destructor (Acari: Varroidae) in Apis mellifera (Hym.: Apidae).Veterinary medicine and science · 2025Article
- In vitro anti-Trichomonas gallinae effects of Ziziphus vulgaris L. and Camellia sinensis (L.) Kuntze extracts.Veterinary medicine and science · 2024Article
- Quercetin as a Promising Antiprotozoan Phytochemical: Current Knowledge and Future Research Avenues.BioMed research international · 2024Review
- Efficacy of the Aqueous Extract ofMolecules (Basel, Switzerland) · 2021Article
- Proposed Mechanism for the Antitrypanosomal Activity of Quercetin and Myricetin Isolated fromMolecules (Basel, Switzerland) · 2021Article
- Article
- Flavonoids as a Natural Treatment AgainstFrontiers in cellular and infection microbiology · 2018Review
- A targeted delivery strategy for the development of potent trypanocides.Chemical communications (Cambridge, England) · 2017Article
- Molecular and biochemical characterization of Eimeria tenella hexokinase.Parasitology research · 2016Article
- A novel high-throughput activity assay for the Trypanosoma brucei editosome enzyme REL1 and other RNA ligases.Nucleic acids research · 2016Article
- Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase.Molecular and biochemical parasitology · 2015Article
- Exploring the mode of action of ebselen in Trypanosoma brucei hexokinase inhibition.International journal for parasitology. Drugs and drug resistance · 2013Article
- Quercetin postconditioning attenuates myocardial ischemia/reperfusion injury in rats through the PI3K/Akt pathway.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologica · 2013Article
- Protective roles of quercetin in acute myocardial ischemia and reperfusion injury in rats.Molecular biology reports · 2012Article
- Glycerol 3-phosphate alters Trypanosoma brucei hexokinase activity in response to environmental change.The Journal of biological chemistry · 2011Article
- Glycolysis in the african trypanosome: targeting enzymes and their subcellular compartments for therapeutic development.Molecular biology international · 2011Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Hexokinases from the African trypanosome, Trypanosoma brucei, are attractive targets for the development of anti-parasitic drugs, in part because the parasite utilizes glycolysis exclusively for ATP production during the mammalian infection. Here, we have demonstrated that the bioflavanoid quercetin (QCN), a known trypanocide, is a mixed inhibitor of Trypanosoma brucei hexokinase 1 (TbHK1) (IC(50) = 4.1 ± 0.8μM). Spectroscopic analysis of QCN binding to TbHK1, taking advantage of the intrinsically fluorescent single tryptophan (Trp177) in TbHK1, revealed that QCN quenches emission of Trp177, which is located near the hinge region of the enzyme. ATP similarly quenched Trp177 emission, while glucose had no impact on fluorescence. Supporting the possibility that QCN toxicity is a consequence of inhibition of the essential hexokinase, in live parasites QCN fluorescence localizes to glycosomes, the subcellular home of TbHK1. Additionally, RNAi-mediated silencing of TbHK1 expression expedited QCN induced death, while over-expressing TbHK1 protected trypanosomes from the compound. In summary, these observations support the suggestion that QCN toxicity is in part attributable to inhibition of the essential TbHK1.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.